Failure of cannabinoid compounds to stimulate estrogen receptors

Biochemical Pharmacology
M F RuhW V Welshons

Abstract

delta 9-Tetrahydrocannabinol (THC), the primary active compound in Cannabis sativa (marihuana), and other cannabinoid receptor agonists exert potent effects on luteinizing hormone and prolactin release in animal models and humans. Compounds possessing the tricyclic cannabinoid structure, including delta 9-THC and cannabidiol, have been reported to interact with rodent uterine estrogen receptors in ligand binding assays. The present study tested the hypothesis that cannabinoid compounds produce a direct activation of estrogen receptors. We investigated whether cannabinoid compounds exhibit estrogen-induced mitogenesis in MCF-7 breast cancer cells. Under conditions in which 10 pM estradiol promoted MCF-7 cell proliferation, no response was observed with biologically relevant concentrations (< = 10 microM) of delta 9-THC or its tricyclic analog desacetyllevonantradol. No response was observed with cannabidiol, a bicyclic cannabinoid compound that exhibits no cannabimimetic behavioral effects but has been reported to bind to the estrogen receptor in vitro. delta 9-THC also failed to antagonize the response to estradiol under conditions in which the antiestrogen LY156758 (keoxifene; raloxifene) was effective. The phytoestrogen formo...Continue Reading

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Citations

Jan 6, 2006·Archives of Pharmacal Research·Soo Yeun LeeKyu Hyuck Chung
Feb 6, 2003·Archives of Pharmacal Research·Chungsook KimSie Won Park
Dec 20, 2003·Prostaglandins, Leukotrienes, and Essential Fatty Acids·Boram ParkMichelle Glass
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Feb 29, 2020·Cancers·Luka DobovišekNataša Debeljak
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Jul 3, 2021·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Ishtiaq AhmedQingyou Liu

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